942507-42-8

AZ304 is potent dual BRAF inhibitor. Is a combination of MEK and B-raf inhibitors for treatment of cancer.

AZ304 is a synthetic inhibitor targeting wild-type and V600E mutant BRAF with IC50 of 79 nM and 38 nM, respectively. It also inhibits CRAF, p38 and CSF1R with IC50 below 100 nM.

AZ304 inhibited wild-type BRAF and CRAF, BRAF in vitro.

In both RKO and Caco-2 tumor models, administration of AZ304 alone or in combination with Cetuximab resulted in antitumor activity without apparent toxic effects (regardless of BRAF mutation).

< td style="border-bottom: 1px dotted #ccc;padding: 5px;"> BRAF(V600E)
(Cell-free assay) < /tr>

Target	Value
p38 (Cell-free assay)	6 nM
CSF1R (Cell-free assay)	35 nM
38 nM
CRAF (Cell-free assay )	68 nM
WT BRAF (Cell-free assay)	79 nM